Dacomitinib (PF299804, PF299) , ≥99% , 1110813-31-4

Synonym(s):
(2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide;PF-00299804;PF-00299804-03;PF-299

CAS NO.：1110813-31-4

Empirical Formula: C24H25ClFN5O2

Molecular Weight: 469.94

MDL number: MFCD19443734

PRODUCT Properties

• Melting point: 184-187°C
• Boiling point: 665.7±55.0 °C(Predicted)
• Density: 1.344
• storage temp.: Refrigerator
• solubility: DMSO (Slightly), Methanol (Slightly, Heated)
• form: White solid.
• pka: 12.05±0.43(Predicted)
• color: White to Pale Yellow

Description and Uses

The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer. PF-299804 is a second generation pan-ErbB receptor tyrosine kinase inhibitor (IC₅₀s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors. At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.

Dacomitinib is an Erb-inhibitor, or an inhibitor of the members of the epidermal growth factor receptor family. Used as an ant-cancer agent due to observation of over-expressed epidermal growth factor receptor in nearly all cases of squamous cell carcinoma in the head and neck.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P280-P305+P351+P338
• HS Code: 29335990